发明授权
- 专利标题: Process for preparing haloketo acid derivatives
- 专利标题(中): 制备卤代酸衍生物的方法
-
申请号: US651971申请日: 1991-02-07
-
公开(公告)号: US5202467A公开(公告)日: 1993-04-13
- 发明人: Takaharu Ikeda , Seiichi Kai , Masayoshi Minai
- 申请人: Takaharu Ikeda , Seiichi Kai , Masayoshi Minai
- 申请人地址: JPX Osaka
- 专利权人: Sumitomo Chemical Company, Limited
- 当前专利权人: Sumitomo Chemical Company, Limited
- 当前专利权人地址: JPX Osaka
- 优先权: JPX2-30013 19900208; JPX2-30014 19900208
- 主分类号: C07C67/313
- IPC分类号: C07C67/313 ; C07C67/343 ; C07C69/716 ; C07C251/38
摘要:
Process for preparing haloketo acid derivatives [I]: ##STR1## wherein R is H or C.sub.1-6 alkyl, and X is chlorine or bromine, which comprises reacting .beta.-oxo-acid ester [II]: ##STR2## wherein R.sup.1 is C.sub.1-6 alkyl, R.sup.2 is C.sub.1-5 alkyl or OR.sup.3 (R.sup.3 is C.sub.1-6 alkyl), and X is the same as above, with nitrosating agent [IV]:ONOR.sup.4 [IV]wherein R.sup.4 is H, alkyl, halogen or SO.sub.3 H to give 7-halo-2-hydroxyiminoheptanoic acid ester [III]: ##STR3## wherein R.sup.1 and X are the same as above, followed by reacting the product with aldehyde or ketone; and intermediates therefor, and process for preparing said intermediates. Said haloketo acid derivatives are useful as intermediate for synthesis of cilastatin, which is useful as medicament, especially as dehydropeptidase inhibitor.